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Technical details about NCGC00024994-06, learn more about the structure, uses, toxicity, action, side effects and more

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2D Structure
Also known as: 14611-52-0, Eldepryl, Selegiline hcl, Zelapar, L-deprenyl hydrochloride, (-)-deprenyl hydrochloride
Molecular Formula
C13H18ClN
Molecular Weight
223.74  g/mol
InChI Key
IYETZZCWLLUHIJ-UTONKHPSSA-N
FDA UNII
6W731X367Q

A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.
1 2D Structure

2D Structure

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(2R)-N-methyl-1-phenyl-N-prop-2-ynylpropan-2-amine;hydrochloride
2.1.2 InChI
InChI=1S/C13H17N.ClH/c1-4-10-14(3)12(2)11-13-8-6-5-7-9-13;/h1,5-9,12H,10-11H2,2-3H3;1H/t12-;/m1./s1
2.1.3 InChI Key
IYETZZCWLLUHIJ-UTONKHPSSA-N
2.1.4 Canonical SMILES
CC(CC1=CC=CC=C1)N(C)CC#C.Cl
2.1.5 Isomeric SMILES
C[C@H](CC1=CC=CC=C1)N(C)CC#C.Cl
2.2 Other Identifiers
2.2.1 UNII
6W731X367Q
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Deprenalin

2. Deprenil

3. Deprenyl

4. E 250

5. E-250

6. E250

7. Eldepryl

8. Emsam

9. Humex

10. Jumex

11. L-deprenyl

12. Selegiline

13. Selegiline Hydrochloride, (r)-isomer

14. Selegiline Hydrochloride, (r,s)-isomer

15. Selegiline Hydrochloride, (s)-isomer

16. Selegiline, (r)-isomer

17. Selegiline, (r,s)-isomer

18. Selegiline, (s)-isomer

19. Selegyline

20. Yumex

21. Zelapar

2.3.2 Depositor-Supplied Synonyms

1. 14611-52-0

2. Eldepryl

3. Selegiline Hcl

4. Zelapar

5. L-deprenyl Hydrochloride

6. (-)-deprenyl Hydrochloride

7. L-deprenyl

8. Ensam

9. (r)-n-methyl-n-(1-phenylpropan-2-yl)prop-2-yn-1-amine Hydrochloride

10. R-(-)-deprenyl Hydrochloride

11. Jumex

12. R-(-)-deprenyl (hydrochloride)

13. R(-)-deprenyl Hydrochloride

14. (r)-(-)-deprenyl Hydrochloride

15. (-)-phenylisopropylmethylpropynylamine

16. Otrasel

17. 6w731x367q

18. Nsc-759259

19. Benzeneethanamine, N,alpha-dimethyl-n-2-propyn-1-yl-, Hydrochloride (1:1), (alphar)-

20. Dsstox_cid_24584

21. Dsstox_rid_80331

22. Jumex Hydrochloride

23. Dsstox_gsid_44584

24. Eldepryl Hydrochloride

25. Zydis Selegiline

26. (2r)-n-methyl-1-phenyl-n-prop-2-ynylpropan-2-amine;hydrochloride

27. Chebi:9087

28. (-)-deprenil Hydrochloride

29. (-)-e-250 Hydrochloride

30. Smr000449328

31. Selegiline Hydrochloride [usan]

32. Hsdb 7183

33. Fpf1100

34. Sr-01000597928

35. Plurimen

36. Seledat

37. Vivapryl

38. Xilopar

39. Ccris 8571

40. Unii-6w731x367q

41. Eldepryl (tn)

42. Prestwick_846

43. (r)-deprenyl Hcl

44. Selegiline Hydrochloride [usan:usp]

45. (-)-(r)-n,alpha-dimethyl-n-2-propynylphenethylamine Hydrochloride

46. (-)-n,alpha-dimethyl-n-2-propynylbenzeneethanamine Hydrochloride

47. Ncgc00016708-01

48. (-)-(r)-n,alpha-dimethyl-n-2-propynylphenethylamine Monohydrochloride

49. Cas-14611-52-0

50. R-(-)deprenyl Hydrochloride

51. Schembl41392

52. (-)-selegiline Hydrochloride

53. Mls000758294

54. Mls001423947

55. Mls002153281

56. Mls002222269

57. Chembl1200904

58. Dtxsid9044584

59. Hms1569p05

60. Fpf-1100

61. Selegiline Hydrochloride (jan/usp)

62. Tox21_110572

63. Tox21_301846

64. (r)-(-)-n,alpha-dimethyl-n-(2-propynyl)phenethylamine Hydrochloride

65. Mfcd00069299

66. Selegiline Hydrochloride [mi]

67. Selegiline Hydrochloride [jan]

68. Akos005166822

69. Benzeneethanamine, N,.alpha.-dimethyl-n-2-propynyl-, Hydrochloride, (r)-

70. Benzeneethanamine, N,alpha-dimethyl-n-2-propynyl-, Hydrochloride, (r)-

71. Tox21_110572_1

72. Ccg-100773

73. Ks-5098

74. Nc00023

75. Nc00605

76. Nsc 759259

77. Selegiline Hydrochloride [hsdb]

78. Selegiline Hydrochloride [mart.]

79. Selegiline Hydrochloride [vandf]

80. Ncgc00024994-06

81. Ncgc00255797-01

82. Selegiline Hydrochloride [usp-rs]

83. Selegiline Hydrochloride [who-dd]

84. Ac-18759

85. Hy-14199

86. Selegiline Hydrochloride [green Book]

87. Selegiline Hydrochloride [orange Book]

88. D00785

89. Selegiline Hydrochloride [ep Monograph]

90. Selegiline Hydrochloride [usp Monograph]

91. 611s520

92. Sr-01000597928-1

93. Sr-01000597928-5

94. Sr-01000597928-6

95. Q27108267

96. R-(-)-deprenyl Hydrochloride, Powder, >=98% (hplc)

97. Selegiline Hydrochloride 1.0 Mg/ml In Methanol (as Free Base)

98. (r)-(-)-n,alpha-dimethyl-n-(2-propynyl)phenethylamine Hcl

99. (r)-(-)-n-?-dimethyl-n-2-propynylbenzeneethanamine Hydrochloride

100. (r)-n-methyl-1-phenyl-n-prop-2-ynylpropan-2-amine Hydrochloride

101. (-)-(r)-n,.alpha.-dimethyl-n-2-propynylphenethylamine Hydrochloride

102. Selegiline Hydrochloride, European Pharmacopoeia (ep) Reference Standard

103. Benzeneethanamine, N,?-dimethyl-n-2-propyn-1-yl-, Hydrochloride (1:1), (?r)-

104. Selegiline Hydrochloride, United States Pharmacopeia (usp) Reference Standard

2.4 Create Date
2005-06-24
3 Chemical and Physical Properties
Molecular Weight 223.74 g/mol
Molecular Formula C13H18ClN
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count1
Rotatable Bond Count4
Exact Mass223.1127773 g/mol
Monoisotopic Mass223.1127773 g/mol
Topological Polar Surface Area3.2 Ų
Heavy Atom Count15
Formal Charge0
Complexity195
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count2
4 Drug and Medication Information
4.1 Drug Information
1 of 6  
Drug NameEldepryl
Drug LabelELDEPRYL (selegiline hydrochloride) is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl.The chemical name is: (R)-(-)-N,2-dimethyl-N-2-propynylphenethylami...
Active IngredientSelegiline hydrochloride
Dosage FormCapsule
RouteOral
Strength5mg
Market StatusPrescription
CompanySomerset

2 of 6  
Drug NameSelegiline hydrochloride
PubMed HealthSelegiline (By mouth)
Drug ClassesAntiparkinsonian
Drug LabelSelegiline hydrochloride is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl. The chemical name is: (R)-(-)-N,2-dimethyl-N-2-propynylphenethylamine hydroch...
Active IngredientSelegiline hydrochloride
Dosage FormTablet; Capsule
RouteOral
Strength5mg
Market StatusPrescription
CompanyApotex; Stason; Dava Pharms; Mylan

3 of 6  
Drug NameZelapar
PubMed HealthSelegiline
Drug ClassesAntidepressant, Antiparkinsonian
Drug LabelZELAPAR Orally Disintegrating Tablets contain selegiline hydrochloride, a levorotatory acetylenic derivative of phenthylamine. Selegiline hydrochloride is described chemically as: (-)-(R)-N, -dimethyl-N-2-propynylphenethylamine hydrochloride and it...
Active IngredientSelegiline hydrochloride
Dosage FormTablet, orally disintegrating
RouteOral
Strength1.25mg
Market StatusPrescription
CompanyValeant Pharm Intl

4 of 6  
Drug NameEldepryl
Drug LabelELDEPRYL (selegiline hydrochloride) is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl.The chemical name is: (R)-(-)-N,2-dimethyl-N-2-propynylphenethylami...
Active IngredientSelegiline hydrochloride
Dosage FormCapsule
RouteOral
Strength5mg
Market StatusPrescription
CompanySomerset

5 of 6  
Drug NameSelegiline hydrochloride
PubMed HealthSelegiline (By mouth)
Drug ClassesAntiparkinsonian
Drug LabelSelegiline hydrochloride is a levorotatory acetylenic derivative of phenethylamine. It is commonly referred to in the clinical and pharmacological literature as l-deprenyl. The chemical name is: (R)-(-)-N,2-dimethyl-N-2-propynylphenethylamine hydroch...
Active IngredientSelegiline hydrochloride
Dosage FormTablet; Capsule
RouteOral
Strength5mg
Market StatusPrescription
CompanyApotex; Stason; Dava Pharms; Mylan

6 of 6  
Drug NameZelapar
PubMed HealthSelegiline
Drug ClassesAntidepressant, Antiparkinsonian
Drug LabelZELAPAR Orally Disintegrating Tablets contain selegiline hydrochloride, a levorotatory acetylenic derivative of phenthylamine. Selegiline hydrochloride is described chemically as: (-)-(R)-N, -dimethyl-N-2-propynylphenethylamine hydrochloride and it...
Active IngredientSelegiline hydrochloride
Dosage FormTablet, orally disintegrating
RouteOral
Strength1.25mg
Market StatusPrescription
CompanyValeant Pharm Intl

4.2 Therapeutic Uses

Monamine oxidase B inhibitor

O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. 13th Edition, Whitehouse Station, NJ: Merck and Co., Inc., 2001., p. 1512


Selegiline is indicated for use with levodopa or levodopa and carbidopa combination in the treatment of idiopathic Parkinson's disease (paralysis agitans). /Included in US product labeling/ /Selegiline/

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442


.... we report briefly on neurotoxicity associated with the immunodeficiency virus and discuss the effects of selegiline, a monoamine oxidase inhibitor which enhances dopamine availability in CNS on immunodeficiency virus-induced neurological disease. ... /MAO inhibitors may be potent mediators of the neuropathological deficits in immunodeficiency virus infection and factors which may accelerate the progression of the immunodeficiency virus --neurological disease./

PMID:14697901 Koutsilieri E et al; Neurotoxicology 25 (1-2): 267-70 (2004)


EXPTL Therapy: ... Twenty patients with mild-moderate pathological cerebral involution of atrophic and/or vascular origin, were treated with Selegiline (L-deprenyl), a monoamino-oxidase B inhibitor (10 mg/day for six months). Compared with a control group, Selegiline treated patients showed a statistically significant improvement in cognitive and behaviour capacities. At the end of investigation, "Mini Mental State" showed an improvement of 26.5% in Selegiline group and of 3.7% in control group (P < 0.01). "Echelle Clinique d'Aptitudes Intellectuelles" showed an improvement of 29.4% and of 10.8% respectively (P < 0.01). Selegiline treatment has shortened significantly the reaction times and has improved mnesic capacities. No side effects were observed during the study. /Selegiline/

PMID:12645393 Bettini R, Gorini M; Clin Ter 153 (6): 377-80 (2002)


For more Therapeutic Uses (Complete) data for SELEGILINE HYDROCHLORIDE (10 total), please visit the HSDB record page.


4.3 Drug Warning

Pregnancy risk category: C /RISK CANNOT BE RULED OUT. Adequate, well controlled human studies are lacking, and animal studies have shown risk to the fetus or are lacking as well. There is a chance of fetal harm if the drug is given during pregnancy; but the potential benefits may outweigh the potential risk./

Physicians Desk Reference. 58th ed. Thomson PDR. Montvale, NJ 2004., p. 3176


Selegiline may decrease or inhibit salivary flow, thus contributing to the development of caries, periodontal disease, oral candidiasis, and discomfort.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2443


Therapeutic use may lead to increased tremor, bradykinesia, falling, dystonic symptoms, dyskinesias, hallucinations, confusion, sleep disturbance, headache, dry mouth, blurred vision, orthostatic hypotension, hypertension, poor appetite, urinary retention, and diaphoresis. Hypomanic behavior may be due to the l-amphetamine and l-amphetamine metabolites of selegiline.

Ellenhorn, M.J., S. Schonwald, G. Ordog, J. Wasserberger. Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore, MD: Williams and Wilkins, 1997., p. 659


In patients receiving levodopa, addition of selegiline hydrochloride may exacerbate levodopa-associated dyskinesias. This effect, which occurred in an average of 28% (range: 4-90%) of patients receiving the drug in clinical trials, usually occurs within 2 weeks after initiating selegiline therapy and generally is mitigated when the levodopa dosage is reduced ... . Involuntary movements, increased tremor, chorea, loss of balance, freezing, blepharospasm, increased bradykinesia, facial grimacing, speech problems, heavy leg, stiff neck, tardive dyskinesia, dystonic manifestations, festination, increased apraxia, and muscle cramping may occur in patients receiving selegiline. Bruxism, muscle twitching and myoclonic jerks have occurred in patients receiving levodopa and selegiline hydrochloride dosages exceeding 10 mg daily.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2439


For more Drug Warnings (Complete) data for SELEGILINE HYDROCHLORIDE (12 total), please visit the HSDB record page.


5 Pharmacology and Biochemistry
5.1 MeSH Pharmacological Classification

Antidepressive Agents

Mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions. Several MONOAMINE OXIDASE INHIBITORS are useful as antidepressants apparently as a long-term consequence of their modulation of catecholamine levels. The tricyclic compounds useful as antidepressive agents (ANTIDEPRESSIVE AGENTS, TRICYCLIC) also appear to act through brain catecholamine systems. A third group (ANTIDEPRESSIVE AGENTS, SECOND-GENERATION) is a diverse group of drugs including some that act specifically on serotonergic systems. (See all compounds classified as Antidepressive Agents.)


Monoamine Oxidase Inhibitors

A chemically heterogeneous group of drugs that have in common the ability to block oxidative deamination of naturally occurring monoamines. (From Gilman, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p414) (See all compounds classified as Monoamine Oxidase Inhibitors.)


Neuroprotective Agents

Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids. (See all compounds classified as Neuroprotective Agents.)


Antiparkinson Agents

Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists. (See all compounds classified as Antiparkinson Agents.)


5.2 FDA Pharmacological Classification
5.2.1 Pharmacological Classes
Monoamine Oxidase Inhibitors [MoA]; Monoamine Oxidase Type B Inhibitor [EPC]; Monoamine Oxidase-B Inhibitors [MoA]; Monoamine Oxidase Inhibitor [EPC]
5.3 Absorption, Distribution and Excretion

Selegiline and its metabolites are widely distributed into body tissues and cross the blood-brain barrier. Following IV administration of radiolabeled selegiline hydrochloride in mice, the parent drug and/or metabolites are rapidly and widely distributed to brain, liver, kidney, lung, heart, and brown fat. Following IV administration of radiolabeled selegiline hydrochloride in healthy adults, the highest accumulation of radioactivity occurred in the thalamus, basal ganglia, mesencephalon, and cingulate gyrus. /Selegiline/

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2441


Selegiline is excreted principally in urine as conjugated and unconjugated metabolites. About 20-63% of an orally administered dose of selegiline is excreted in urine as l-methamphetamine, 9-26% as l-amphetamine, and 1% as l-demethylselegiline. ... About 15% of a dose is excreted in feces within 72 hours following administration of selegiline. /SRP: This would usually result in a false positive drug test for d-methamphetamine if no d/l-isomer characterization was performed on the specimen./ /Selegiline/

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2441


Rapidly absorbed from the gastrointestinal tract.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442


... The mean peak plasma concentration (Cmax) is approximately 2 ug/L and the time to reach the peak is under an hour. The absolute bioavailability of selegiline is approximately 10%. It has an apparent volume of distribution of 1854 L. The oral clearance of selegiline (59 L/min) is many fold higher than the liver blood flow (1.5 L/min), indicating that extrahepatic processes are involved in the elimination of selegiline. ... /Selegiline/

PMID:9260033 Mahmood I; Clin Pharmacokinet 33 (2): 91-102 (1997)


... Selegiline is readily absorbed from the gastrointestinal tract and rapidly enters the brain and spinal cord following oral administration. The drug binds to brain regions with a high MAO-B content, such as the thalamus, the striatum, the cortex, and the brainstem. ... /Selegiline/

Gerlach M et al; Neurology 47 (6 Suppl 3): S137-45 (1996)


5.4 Metabolism/Metabolites

Selegiline is excreted principally in urine as conjugated and unconjugated metabolites. About 20-63% of an orally administered dose of selegiline is excreted in urine as l-methamphetamine, 9-26% as l-amphetamine, and 1% as l-demethylselegiline. /Selegiline/

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2441


Rapidly and completely metabolized to N-desmethyldeprenyl, l-methamphetamine, and l-amphetamine.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442


Selegiline is extensively metabolized, presumably through cytochrome p450 mediated oxygenation, to form l-desmethylselegiline and l-methamphetamine, which is further metabolized to l-amphetamine. Selegiline also is metabolized in the lungs to l-desmethylselegiline and l-methamphetamine and in the kidneys to l-methamphetamine, but the degree of metabolism in these tissues is minimal compared with that in the liver. /Selegiline/

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 2441


... The pharmacokinetics of selegiline are highly variable. Following an oral dose of selegiline 10 mg, it is rapidly absorbed and metabolized to desmethylselegiline, levoamphetamine and levomethamphetamine. /Selegiline/

PMID:9260033 Mahmood I; Clin Pharmacokinet 33 (2): 91-102 (1997)


For more Metabolism/Metabolites (Complete) data for SELEGILINE HYDROCHLORIDE (6 total), please visit the HSDB record page.


5.5 Biological Half-Life

Elimination: Selegiline: 39 (range, 16 to 69) hours. /Selegiline/

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442


The mean half-lives of the 3 active metabolites that were found in serum and urine following a single dose of selegiline are as follows: N-desmethyldeprenyl, 2 hours; l-amphetamine, 17.7 hours; l-methamphetamine, 20.5 hours. /Selegiline/

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442


5.6 Mechanism of Action

The action of selegiline is thought to be related to its irreversible inhibition of monoamine oxidase type B (MAO B), the major form of the enzyme in the human brain. MAO B, which is involved in the oxidative deamination of dopamine in the brain, is inhibited when selegiline binds covalently and stoichiometrically to the isoalloxazine flavin adenine dinucleotide (FAD) at its active center. Administration of 10 mg of selegiline a day produces almost complete inhibition of MAO B in the brain. Selegiline becomes a nonselective inhibitor of all monamine oxidase (MAO) at higher doses, possibly at 20 to 40 mg a day. At these doses, tyramine-mediated hypertensive reaction with MAO A blockade ("cheese reactions") may occur. /Selegiline/

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442


Selegiline (or its metabolites) may also act through other mechanisms to increase dopaminergic activity, including interfering with dopamine reuptake at the synapse. /Selegiline/

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2442


The mechanism of action of selegiline is complex and cannot be explained solely by its MAO-B inhibitory action. Pretreatment with selegiline can protect neurons against a variety of neurotoxins, such as 1-methyl-4-phenyl-1,2,3,6 tetrahydropyridine (MPTP), 6-hydroxydopamine, N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP-4), methyl-beta-acetoxyethyl-2-chloroethylamine (AF64A), and 5,6-dihydroxyserotonin, which damage dopaminergic, adrenergic, cholinergic, and sertoninergic neurons, respectively. Selegiline produces an amphetamine-like effect, enhances the release of dopamine, and blocks the reuptake of dopamine. It stimulates gene expression of L-aromatic amino acid decarboxylase, increases striatal phenylethylamine levels, and activates dopamine receptors. Selegiline reduces the production of oxidative radicals, up-regulates superoxide dismutase and catalase, and suppresses nonenzymatic and iron-catalyzed autooxidation of dopamine. Selegiline compensates for loss of target-derived trophic support, delays apoptosis in serum-deprived cells, and blocks apoptosis-related fall in the mitochondrial membrane potential. Most of the aforementioned properties occur independently of selegiline's efficacy to inhibit MAO-B. /Selegiline/

PMID:11813232 Ebadi M et al; J Neurosci Res 67 (3): 285-9 (2002)


Selegiline is a selective inhibitor of monoamine oxidase-B (MAO-B) at a dose of 10 mg/day and is given to patients with Parkinson's disease as an adjunct to levodopa therapy. By inhibiting MAO-B, selegiline increases the dopamine levels in the substantia nigra. Selegiline also blocks dopamine re-uptake from the synaptic cleft, thus increasing the dopamine concentrations in the brain. ... /Selegiline/

PMID:9260033 Mahmood I; Clin Pharmacokinet 33 (2): 91-102 (1997)


For more Mechanism of Action (Complete) data for SELEGILINE HYDROCHLORIDE (6 total), please visit the HSDB record page.


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